The discovery of aminopyrazines as novel, potent Naᵥ1.7 antagonists: Hit-to-lead identification and SAR
2012
Bregman, Howard | Nguyen, Hanh Nho | Feric, Elma | Ligutti, Joseph | Liu, Dong | McDermott, Jeff S. | Wilenkin, Ben | Zou, Anruo | Huang, Liyue | Li, Xingwen | McDonough, Stefan I. | DiMauro, Erin F.
Herein the discovery of a novel class of aminoheterocyclic Naᵥ1.7 antagonists is reported. Hit compound 1 was potent but suffered from poor pharmacokinetics and selectivity. The compact structure of 1 offered a modular synthetic strategy towards a broad structure–activity relationship analysis. This analysis led to the identification of aminopyrazine 41, which had vastly improved hERG selectivity and pharmacokinetic properties.
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